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Encyclopedia > Propofol
Propofol
Systematic (IUPAC) name
2,6-diisopropylphenol
Identifiers
CAS number 2078-54-8
ATC code N01AX10
PubChem 4943
DrugBank APRD01201
Chemical data
Formula C12H18O 
Mol. mass 178.271 g/mol
Pharmacokinetic data
Bioavailability NA
Protein binding 95 to 99%
Metabolism Hepatic glucuronidation
Half life 30 to 60 min
Excretion Renal
Therapeutic considerations
Pregnancy cat.

B (U.S.), C (Au) Image File history File links Download high-resolution version (1100x723, 14 KB) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Propofol ... Image File history File links Download high-resolution version (1358x1000, 173 KB) File links The following pages on the English Wikipedia link to this file (pages on other projects are not listed): Propofol ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article or section does not cite any references or sources. ... General Name, Symbol, Number carbon, C, 6 Chemical series nonmetals Group, Period, Block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... BIC pen cap, about 1 gram. ... The mole (symbol: mol) is the SI base unit that measures an amount of substance. ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ present in vertebrates and some other animals. ... Example of glucuronidation Glucuronidation of alcohols and acids Glucuronidation is a major inactivating pathway for a huge variety of exogenous and endogenous molecules, including drugs, polluants, bilirubin, androgens, estrogens, mineralocorticoids, glucocorticoids, fatty acid derivatives, retinoids and bile acids. ... It has been suggested that Effective half-life be merged into this article or section. ... A minute is a unit of time equal to 1/60th of an hour and to 60 seconds. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The kidneys are organs that filter wastes (such as urea) from the blood and excrete them, along with water, as urine. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from... Anthem Advance Australia Fair Royal anthem: God Save the Queen Capital Canberra Largest city Sydney Official languages English (de facto 1) Government Federal constitutional monarchy and parliamentary democracy  -  Queen Elizabeth II  -  Governor-General Michael Jeffery  -  Prime Minister John Howard Independence from the United Kingdom   -  Constitution 1 January 1901   -  Statute of...

Legal status

℞-only (U.S.) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained. ...

Routes Intravenous

Propofol is a short-acting intravenous anesthetic agent used for the induction of general anesthesia in adult patients and pediatric patients older than 3 years of age; maintenance of general anesthesia in adult patients and pediatric patients older than 2 months of age; and sedation in medical contexts, such as intensive care unit (ICU) sedation for intubated, mechanically ventilated adults, and in procedures such as colonoscopy. It provides no analgesia. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Intravenous therapy or IV therapy is the giving of liquid substances directly into a vein. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Anesthesia or anaesthesia (see spelling differences) has traditionally meant the condition of having the perception of pain and other sensations blocked. ... Sedation is a medical procedure involving administration of sedative drugs, generally to facilitate a medical procedure, such as endoscopy, vasectomy, or minor surgery with local anaesthesia. ... An intensive care unit An Intensive Care Unit (ICU) or Critical Care Unit (CCU) is a specialised facility in a hospital that provides intensive care medicine. ... Colonoscopy is the minimally invasive endoscopic examination of the large colon and the distal part of the small bowel with a CCD camera or a fiber optic camera on a flexible tube passed through the anus. ... For other uses of painkiller, see painkiller (disambiguation) An analgesic (colloquially known as painkiller) is any member of the diverse group of drugs used to relieve pain. ...


Propofol is approved for the induction and maintenance of anesthesia in more than 50 countries.


It is also commonly used in veterinary medicine and many veterinary anaesthetists regard it as the induction agent of choice for small animals (dogs, cats etc) as it can be administered to effect, reducing the risk of accidental overdose. Veterinary medicine is the application of medical, diagnostic, and therapeutic principles to companion, domestic, exotic, wildlife, and production animals. ... Veterinary anesthesia is anesthesia performed on animals (excluding humans) performed by a veterinarian. ... Trinomial name Canis lupus familiaris The dog (Canis lupus familiaris) is a domestic subspecies of the wolf, a mammal of the Canidae family of the order Carnivora. ... Binomial name Felis catus Linnaeus, 1758 Synonyms Felis lybica invalid junior synonym The cat (or domestic cat, house cat) is a small carnivorous mammal. ...

Contents

Chemistry

20 ml ampoule of 1% propofol emulsion

Propofol is a water-immiscible oil and so cannot be injected per se. Initial clinical trials were in 1977, in a form solubilised in cremophor EL, but due to anaphylactic reactions it was withdrawn from the market. It was subsequently reformulated as an emulsion of a soya oil/propofol mixture in water, and re-launched in 1986 by AstraZeneca with the brand name Diprivan (shortened version of DI-isoPRopyl IV ANesthetic). The current preparation is 1% propofol, 10% soybean oil and 1.2% purified egg phospholipid (emulsifier), with 2.25% of glycerol as a tonicity adjusting agent, and sodium hydroxide to adjust the pH. Diprivan contains EDTA as an antimicrobial agent. Newer generic formulations contain sodium metabisulfite or benzyl alcohol. Propofol emulsion appears as a highly opaque white fluid due to the scattering of light from the tiny (~150 nm) oil droplets that it contains. 20ml ampule of propofol This image has been released into the public domain by the copyright holder, its copyright has expired, or it is ineligible for copyright. ... 20ml ampule of propofol This image has been released into the public domain by the copyright holder, its copyright has expired, or it is ineligible for copyright. ... A. Two immisicible liquids, not emulsified; B. An emulsion of Phase B dispersed in Phase A; C. The unstable emulsion progressively separates; D. The surfactant (purple outline) positions itself on the interfaces between Phase A and Phase B, stabilizing the emulsion An emulsion is a mixture of two immiscible (unblendable... Cremophor EL is polyethoxylated castor oil. ... Anaphylaxis is an acute systemic (multi-system) and severe Type I Hypersensitivity allergic reaction. ... A. Two immisicible liquids, not emulsified; B. An emulsion of Phase B dispersed in Phase A; C. The unstable emulsion progressively separates; D. The surfactant (purple outline) positions itself on the interfaces between Phase A and Phase B, stabilizing the emulsion An emulsion is a mixture of two immiscible (unblendable... AstraZeneca PLC (LSE: AZN, NYSE: AZN), is a large Anglo-Swedish pharmaceutical company formed on 6 April 1999 by the merger of Swedish Astra AB and British Zeneca Group. ... Tonicity is a measure of effective osmolarity or effective osmolality. ... EDTA is a widely-used acronym for the chemical compound ethylenediamine tetraacetic acid (and many other names, see table). ... Sodium metabisulfite or sodium pyrosulfiteis a sterilizer and antioxidant/preservative. ... Benzyl alcohol, also known as phenylmethanol, is a clear, colorless liquid with a mild pleasant aromatic odor. ...


Pharmacology

Propofol is highly protein bound in vivo and is metabolised by conjugation in the liver. Its rate of clearance exceeds hepatic blood flow, suggesting an extrahepatic site of elimination as well. Its mechanism of action is uncertain, but it is postulated that its primary effect may be potentiation of the GABA-A receptor, possibly by slowing the closing channel time. Recent research has also suggested the endocannabinoid system may contribute significantly to Propofol's anesthetic action and to its unique properties.[1] The GABAA receptor is one of the three ligand-gated ion channels responsible for mediating the effects of Gamma-AminoButyric Acid (GABA), the major inhibitory neurotransmitter in the brain. ... Cannabinoids are a group of chemicals which activate the bodys cannabinoid receptors. ...


The elimination half-life of propofol has been estimated to be between 2–24 hours. However, its duration of clinical effect is much shorter because propofol is rapidly distributed into peripheral tissues, and its effects therefore wear off considerably within even a half hour of injection. This, together with its rapid effect (within minutes of injection) and the moderate amnesia it induces makes it an ideal drug for IV sedation.


Side effects

Aside from the hypotension (mainly through vasodilatation) and transient apnea following induction doses, one of propofol's most frequent side effects is pain on injection, especially in smaller veins. This pain can be mitigated by pretreatment with lidocaine.[2] Patients tend to show great variability in their response to propofol, at times showing profound sedation with small doses. Apnea (British spelling - apnoea) (Greek απνοια, from α-, privative, πνεειν, to breathe) is a technical term for suspension of external breathing. ... Lidocaine (INN) (IPA: ) or lignocaine (former BAN) (IPA: ) is a common local anesthetic and antiarrhythmic drug. ...


Propofol has been known to cause an adverse reaction in some patients, known cases include myoclonia and dystonia. Note this is extremely rare. Dystonia (literally, abnormal muscle tone) is a generic term used to describe a neurological movement disorder involving involuntary, sustained muscle contractions. ...


Propofol appears to be safe for use in porphyria, and has not been known to trigger malignant hyperpyrexia. It has been suggested that Acute intermittent porphyria be merged into this article or section. ... Malignant hyperthermia is a life-threatening condition resulting from a genetic sensitivity of skeletal muscles to volatile anaesthetics and depolarizing neuromuscular blocking drugs that occurs during or after anaesthesia. ...


One of the most feared long term side effects is the propofol infusion syndrome. This metabolic derangement most often occurs in children after a prolonged infusion with a high dose and is associated with a high mortality.


Trivia

A common hospital-worker slang term for Propofol is "Milk of Amnesia/Milk of Anesthesiologists", the former a pun on Milk of Magnesia, a similarly milky laxative. It is also called "Penguin Milk" by some eminent pediatric anesthesiologists in the UK whilst inducing children ("gets them confused and takes their mind off what's happening"). Milk of Magnesia, or Magnesium Hydroxide, Mg(OH)2 is a saline osmotic (hydrating) laxative. ... Laxatives are foods, compounds, or drugs taken to induce bowel movements, most often taken to treat constipation. ...


References

  1. ^ Fowler, CJ. "Possible involvement of the endocannabinoid system in the actions of three clinically used drugs." Trends Pharmacol. Sci. 2004 Feb;25(2):59-61.
  2. ^ Propofol Drug Information,Professional. drugs.com. Retrieved on 2007-01-02.

Year 2007 (MMVII) is the current year, a common year starting on Monday of the Gregorian calendar and the AD/CE era. ... is the 2nd day of the year in the Gregorian calendar. ...

External links


  Results from FactBites:
 
Propofol (1347 words)
Propofol may be of particular usefulness for use in Greyhounds and in patients with preexisting cardiac dysrhythmias.
In dogs, propofol’s labeled indications are: 1) for induction of anesthesia; 2) for mainte­nance of anesthesia for up to 20 minutes; 3) for induction of general anesthesia where maintenance is provided inhalant anesthetics.
Propofol’s short duration of action is principally due to its rapid redistribution from the CNS to other tissues.
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